Abstract
Restoring p53 activity by inhibiting the interaction between p53 and MDM2 represents an attractive approach for cancer therapy. To this end, a number of small-molecule p53-MDM2 binding inhibitors have been developed during the past several years. Nutlin-3 is a potent and selective small-molecule MDM2 antagonist that has shown considerable promise in pre-clinical studies. This review will highlight recent advances in the development of small-molecule MDM2 antagonists as potential cancer therapeutics, with special emphasis on Nutlin-3.
Publication types
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Research Support, N.I.H., Extramural
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Review
MeSH terms
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Antineoplastic Agents / pharmacology*
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Genes, p53*
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Humans
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Imidazoles / pharmacology*
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Molecular Targeted Therapy
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Piperazines / pharmacology*
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Protein Binding
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Proto-Oncogene Proteins c-mdm2 / antagonists & inhibitors*
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Tumor Suppressor Protein p53 / agonists*
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Tumor Suppressor Protein p53 / metabolism
Substances
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Antineoplastic Agents
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Imidazoles
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Piperazines
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Tumor Suppressor Protein p53
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nutlin 3
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MDM2 protein, human
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Proto-Oncogene Proteins c-mdm2